Smoking substitutes for nasal administration-I

Abstract

A smoking substitute composition for application directly into the nose, consisting essentially of an aqueous solution of nicotine or a physiologically acceptable acid addition salt thereof, having a pH value of 2 to 6, containing 10 to 0.5% w/v of nicotine calculated as the free base, containing a nasally-acceptable thickening agent, and having a viscosity not less than 100 centipoise and optionally containing also a further ingredient selected from the group consisting of a nasally acceptable buffer, emulsifying agent, preservative, flavoring agent and antioxidant. A method of diminishing the desire of a subject to smoke comprising the step of administering to the subject a smoking substitute composition as set forth in the foregoing.

What we claim is: 
     
       1. A smoking substitute composition for application directly into the nose, consisting essentially of an aqueous solution of nicotine or a physiologically acceptable acid addition salt thereof, having a pH value of 2 to 6, containing 10 to 0.5% w/v of nicotine calculated as the free base, containing a nasally-acceptable thickening agent, having a viscosity not less than 100 centipose, and having about 0.5 to 5 mg nicotine per every 0.05 to 0.5 ml thereof. 
     
     
       2. A composition of claim 1 in a unit dosage form comprising 0.05 up to 0.5 ml of said aqueous solution which delivers about 0.5 to 5 mg nicotine per unit dose. 
     
     
       3. A composition of claim 1, having a viscosity not less than 1,000 centipoise. 
     
     
       4. A composition of claim 3, containing an effective amount of nasally-acceptable buffer having a buffering effect in the range of pH 2 to 6. 
     
     
       5. A composition of claim 4, wherein the buffer has a buffering effect in the range of pH 4 to 6. 
     
     
       6. A composition of claim 3, having a viscosity not higher than 6,000 centipoise. 
     
     
       7. A composition of claim 1, wherein the thickening agent is a nasally-acceptable natural or synthetic polymer. 
     
     
       8. A composition of claim 1, wherein the thickening agent is a nasally-acceptable oily substance constituting the oil-phase of an emulsion. 
     
     
       9. A composition of claim 8, also comprising an emulsifying agent. 
     
     
       10. A composition of claim 1, having a pH value of 3 to 5. 
     
     
       11. A composition of claim 1, containing 5 to 1% w/v of nicotine. 
     
     
       12. A composition of claim 11, containing 4 to 2% w/v of nicotine. 
     
     
       13. A composition of claim 1, wherein the aqueous solution is 0.05 up to 0.3 ml. 
     
     
       14. A composition of claim 1, containing also an effective amount of a nasally-acceptable preservative agent. 
     
     
       15. A composition of claim 1, containing also an effective amount of a nasally-acceptable flavoring agent. 
     
     
       16. A composition of claim 1, containing also an effective amount of a nasally-acceptable antioxidant. 
     
     
       17. A composition of claim 2, wherein the composition is in unit dosage form in a disposable plastic container having a nostril-insertable neck portion of restrictive volume adjacent to an emission opening and a pressure-application chamber of a relatively larger volume in communication with said neck portion, wherein the said composition is disposed in said neck portion and of sufficient viscosity to retain said location until the time of application. 
     
     
       18. A composition of claim 17, wherein the nostril-insertable container neck is itself dimensioned so as to contain a unit dose and wherein a squeeze-bottle container constitutes the relatively larger pressure application chamber, the unit dose neck thus constituting a portion of a multi-dose container. 
     
     
       19. A method of diminishing the desire of a subject to smoke, which comprises the step of administering to the subject intranasally a smoking substitute composition according to any one of claims 1 through 18.